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https://www.readbyqxmd.com/read/28633547/lipid-based-nanosystem-of-edaravone-development-optimization-characterization-and-in-vitro-in-vivo-evaluation
#1
Ankit Parikh, Krishna Kathawala, Chun Chuan Tan, Sanjay Garg, Xin-Fu Zhou
Edaravone (EDR) is a well-recognized lipophilic free radical scavenger for diseases including neurodegenerative disease, cardiovascular disease, and cancer. However, its oral use is restricted due to poor oral bioavailability (BA). The aim of present research was to enable its oral use by developing a lipid-based nanosystem (LNS). The components of LNS including oil, surfactants, and co-surfactants were selected based on their potential to maximize the solubilization in gastrointestinal (GI) fluids, reduce its glucuronidation and improve transmembrane permeability...
November 2017: Drug Delivery
https://www.readbyqxmd.com/read/28625343/short-term-cooling-increases-serum-triglycerides-and-small-high-density-lipoprotein-levels-in-humans
#2
Geerte Hoeke, Kimberly J Nahon, Leontine E H Bakker, Sabine S C Norkauer, Donna L M Dinnes, Maaike Kockx, Laeticia Lichtenstein, Diana Drettwan, Anne Reifel-Miller, Tamer Coskun, Philipp Pagel, Fred P H T M Romijn, Christa M Cobbaert, Ingrid M Jazet, Laurent O Martinez, Leonard Kritharides, Jimmy F P Berbée, Mariëtte R Boon, Patrick C N Rensen
BACKGROUND: Cold exposure and β3-adrenergic receptor agonism, which both activate brown adipose tissue, markedly influence lipoprotein metabolism by enhancing lipoprotein lipase-mediated catabolism of triglyceride-rich lipoproteins and increasing plasma high-density lipoprotein (HDL) levels and functionality in mice. However, the effect of short-term cooling on human lipid and lipoprotein metabolism remained largely elusive. OBJECTIVE: The objective was to assess the effect of short-term cooling on the serum lipoprotein profile and HDL functionality in men...
May 3, 2017: Journal of Clinical Lipidology
https://www.readbyqxmd.com/read/28619449/development-of-semisolid-self-microemulsifying-drug-delivery-systems-smeddss-filled-in-hard-capsules-for-oral-delivery-of-aciclovir
#3
Ljiljana Djekic, Jovana Jankovic, Bojan Čalija, Marija Primorac
The study aimed to develop semisolid self-microemulsifying drug delivery systems (SMEDDSs) as carriers for oral delivery of aciclovir in hard hydroxypropylmethyl cellulose (HPMC) capsules. Six self-dispersing systems (SD1-SD6) were prepared by loading aciclovir into the semisolid formulations consisting of medium chain length triglycerides (lipid), macrogolglycerol hydroxystearate (surfactant), polyglyceryl-3-dioleate (cosurfactant), glycerol (hydrophilic cosolvent), and macrogol 8000 (viscosity modifier). Their characterization was performed in order to identify the semisolid system with rheological behaviour suitable for filling in hard HPMC capsules and fast dispersibility in acidic and alkaline aqueous media with formation of oil-in-water microemulsions...
June 12, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28615942/irgd-modified-lipid-polymer-hybrid-nanoparticles-loaded-with-isoliquiritigenin-to-enhance-anti-breast-cancer-effect-and-tumor-targeting-ability
#4
Fei Gao, Jinming Zhang, Chaomei Fu, Xiaoming Xie, Fu Peng, Jieshu You, Hailin Tang, Zhiyu Wang, Peng Li, Jianping Chen
Isoliquiritigenin (ISL), a natural anti-breast cancer dietary compound, has poor delivery characteristics and low bioavailability. In order to promote the therapeutic outcome of ISL, a tumor-targeting lipid-polymer hybrid nanoparticle (NP) system modified by tumor-homing iRGD peptides has been developed. The hybrid NPs were prepared by a modified single-step nanoprecipitation method to encapsulate ISL. iRGD peptides were anchored on the surface by a postinsertion method (ISL-iRGD NPs). The stable lipid-polymer structure of ISL-iRGD NPs, with high encapsulation and loading efficiency, was confirmed...
2017: International Journal of Nanomedicine
https://www.readbyqxmd.com/read/28614069/pegylated-lipid-bilayer-wrapped-nano-graphene-oxides-for-synergistic-co-delivery-of-doxorubicin-and-rapamycin-to-prevent-drug-resistance-in-cancers
#5
Raj Kumar Thapa, Jeong Hoon Byeon, Han-Gon Choi, Chul Soon Yong, Jong Oh Kim
Nano-graphene oxide (nGO) is a carbon allotrope studied for its potential as carrier for chemotherapeutic delivery and its photoablation effects. However, interaction of nGO with blood components and the subsequent toxicities warrant a hybrid system for effective cancer drug delivery. Combination chemotherapy aids in effective cancer treatment and prevention of drug resistance. Therefore, in this study, we attempted to prepare polyethylene glycosylated (PEGylated) lipid bilayer-wrapped nGO co-loaded with doxorubicin (DOX) and rapamycin (RAPA), GOLDR, for the prevention and treatment of resistant cancers...
June 14, 2017: Nanotechnology
https://www.readbyqxmd.com/read/28614063/microfluidic-hydrodynamic-focusing-synthesis-of-polymer-lipid-nanoparticles-for-sirna-delivery
#6
Xueqin Huang, Robert J Lee, Yuhang Qi, Yujing Li, Jiahui Lu, Qingfan Meng, Lesheng Teng, Jing Xie
Small interfering RNAs (siRNAs) are promising as therapeutics for intractable diseases such as cancer. However, efficient and safe delivery of siRNAs in vivo remains a challenge. Polymer-lipid hybrid nanoparticles (P/LNPs) have been evaluated for therapeutic delivery of siRNA. In this study, a microfluidic hydrodynamic focusing (MF) system was used to prepare P/LNPs loaded with VEGF siRNA. P/LNPs made by MF were smaller in particle size and had narrower size distribution compared to P/LNPs formed by bulk mixing (BM)...
May 30, 2017: Oncotarget
https://www.readbyqxmd.com/read/28612562/-pancreatic-%C3%AE-cell-dysfunction-and-apoptosis-induced-by-elevated-free-fatty-acids-synergize-with-hyperglycemia
#7
Hui-Wen Tan, Nai-Qian Zhao, Ye-Rong Yu, Li-Na Han, Xiang-Xun Zhang
OBJECTIVES: To analysis the effects of glucoxicity and lipotoxicity on the function and apoptosis of pancreatic β-cells. METHODS: The levels of circulating glucose and free fat acids (FFAs) were elevated by infusion dextrose and fat emulsion in high-fat obese rats. The insulin resistance model obese rats were divided into four gourp: obese group with saline infusion (OB-NS group, n=7), obese group with glucose infusion (OB-GS group, n=9), obese group with Lipid emulsion infusion (OB-FFA group, n=8), obese group with glucose and lipid emulsion infusion (OB-FG group, n=9)...
January 2017: Sichuan da Xue Xue Bao. Yi Xue Ban, Journal of Sichuan University. Medical Science Edition
https://www.readbyqxmd.com/read/28599673/low-hdl-cholesterol-among-hiv-1-infected-and-hiv-1-uninfected-individuals-in-nairobi-kenya
#8
Anne Njoroge, B L Guthrie, Rose Bosire, Mark Wener, James Kiarie, Carey Farquhar
BACKGROUND: Antiretroviral treatment (ART) is associated with dyslipidemia yet little is known about the burden of dyslipidemia in the absence of ART in sub-Saharan Africa. We compared the prevalence and risk factors for dyslipidemia among HIV-infected ART-naïve adults and their uninfected partners in Nairobi, Kenya. METHODS: Non-fasting total cholesterol (TC) and high density lipoprotein cholesterol (HDL) levels were measured by standard lipid spectrophotometry on thawed plasma samples obtained from HIV-infected participants and their uninfected partners...
June 9, 2017: Lipids in Health and Disease
https://www.readbyqxmd.com/read/28578400/lipid-droplet-associated-hydrolase-promotes-lipid-droplet-fusion-and-enhances-atgl-degradation-and-triglyceride-accumulation
#9
Young-Hwa Goo, Se-Hee Son, Antoni Paul
Lipid droplet (LD)-associated hydrolase (LDAH) is a newly identified LD protein abundantly expressed in tissues that predominantly store triacylglycerol (TAG). However, how LDAH regulates TAG metabolism remains unknown. We found that upon oleic acid loading LDAH translocalizes from the ER to newly formed LDs, and induces LD coalescence in a tubulin-dependent manner. LDAH overexpression and downregulation in HEK293 cells increase and decrease, respectively, TAG levels. Pulse and chase experiments show that LDAH enhances TAG biogenesis, but also decreases TAG turnover and fatty acid release from cells...
June 2, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28578126/ultradeformable-liposome-loaded-with-zinc-phthalocyanine-and-ru-nh-nhq-tpy-no-3-for-photodynamic-therapy-by-topical-application
#10
Renata Galvão de Lima, Antonio Cláudio Tedesco, Roberto Santana da Silva, Margaret Jayne Lawrence
Ultradeformable liposomes (UDLs) as a drug delivery system (DDS), prepared from the unsaturated phospholipid, dioleylphosphocholine (DOPC), and containing the non-ionic surfactant Tween 20 as edge activator, have been explored as topical vehicles for zinc phthalocyanine (ZnPc) and the nitrosyl ruthenium complex [Ru(NH.NHq)(tpy)NO](3+) (RuNO) as a photosensitizers for co-generation of (1)O2 and NO as reactive species, respectively. However, in order to ensure that ZnPc was present in the UDLs in its monomeric form - essential for maximal ZnPc photophysical properties - it was necessary to replace 40wt% of the DOPC with the saturated phospholipid, dimyristoylphosphocholine (DMPC)...
May 31, 2017: Photodiagnosis and Photodynamic Therapy
https://www.readbyqxmd.com/read/28577969/lipid-alginate-nanoparticle-loaded-in-situ-gelling-system-tailored-for-dexamethasone-nasal-delivery
#11
Bisera Jurišić Dukovski, Ivana Plantić, Ivan Čunčić, Iva Krtalić, Marina Juretić, Ivan Pepić, Jasmina Lovrić, Anita Hafner
In this study, we suggest the development of nanoparticle loaded in situ gelling system suitable for corticosteroid nasal delivery. We propose lipid/alginate nanoparticles (size 252.3±2.4nm, polydispersity index 0.241, zeta-potential -31.7±1.0mV, dexamethasone (Dex) content 255±7μgml(-1)) dispersed in pectin solution (5mgml(-1)) that undergoes a sol-gel phase transition triggered by Ca(2+) present in nasal mucosa. The viscoelasticity of gel obtained by mixing nanoparticle suspension in pectin continuous phase with simulated nasal fluid (1:1V/V) is characterized by a log-linear shear thinning viscosity behaviour...
May 31, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28577496/hepatoprotective-and-antioxidant-activity-of-quercetin-loaded-chitosan-alginate-particles-in-vitro-and-in-vivo-in-a-model-of-paracetamol-induced-toxicity
#12
Virginia Tzankova, Denitsa Aluani, Magdalena Kondeva-Burdina, Yordan Yordanov, Feodor Odzhakov, Alexandar Apostolov, Krassimira Yoncheva
The toxic liver impairment caused by free radical injury or excessive reactive oxigen species (ROS) formation could be effectivelly attenuated by natural antioxidants. The present study aimed to explore and compare the hepatoprotective and antioxidant effects of free and encapsulated quercetin in in vitro and in vivo models of hepatotoxicity. Thus, quercetin was encapsulated in chitosan/alginate nanoparticles by gelation method. Both empty and quercetin-loaded nanoparticles revealed good safety profile in vitro, determined by the lack of cytotoxicity in human hepatoma HepG2 cells...
May 31, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28577126/nanoencapsulation-improves-scavenging-capacity-and-decreases-cytotoxicity-of-silibinin-and-pomegranate-oil-association
#13
Marila C L Marchiori, Cristina Rigon, Priscila M Copetti, Michele R Sagrillo, Letícia Cruz
Silibinin (SB) and pomegranate oil (PO) present therapeutic potential due to antioxidant activity, but the biological performance of both bioactives is limited by their low aqueous solubility. To overcome this issue, the aim of the present investigation was to develop nanocapsule suspensions with PO as oil core for SB encapsulation, as well as assess their toxicity in vitro and radical scavenging activity. The nanocapsule suspensions were prepared by interfacial deposition of preformed polymer method. SB-loaded PO-based nanocapsules (SBNC) showed an average diameter of 157 ± 3 nm, homogenous size distribution, zeta potential of -14...
June 2, 2017: AAPS PharmSciTech
https://www.readbyqxmd.com/read/28576551/free-paclitaxel-loaded-e-selectin-binding-peptide-modified-micelle-self-assembled-from-hyaluronic-acid-paclitaxel-conjugate-inhibit-breast-cancer-metastasis-in-a-murine-model
#14
Xiaofeng Han, Xuerong Dong, Jing Li, Manyuan Wang, Lei Luo, Zhaoxia Li, Xuran Lu, Rui He, Rongsong Xu, Muxin Gong
The present work seeks to construct a nanovehicle for the efficient suppression of breast cancer metastasis through targeting E-selectin on tumor vascular endothelial cells and hyaluronic acid-receptor on tumor cells. Herein, a new ligand-PEG-lipid conjugate, E-selectin binding peptide-polyethene glycol-1-octadecylamine (Esbp-PEG-OA), was used as the targeting molecule of micelle self-assembled form hyaluronic acid-paclitaxel (HA-PTX) conjugate. When loaded with free PTX, the micelles (Esbp-HA-PTX/PTX) exhibited nanoscale particle size with high drug-loading capacity (up to 31...
May 31, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28575449/efficacy-of-a-poly-aggregated-formulation-of-amphotericin-b-in-treating-systemic-sporotrichosis-caused-by-sporothrix-brasiliensis
#15
Kelly Ishida, Rafaela Alves Castro, Juan J Torrado, Dolores Remedios Serrano, Luana Pereira Borba-Santos, Leonardo Pereira Quintella, Wanderley de Souza, Sonia Rozental, Leila M Lopes-Bezerra
In severe cases of sporotrichosis, it is recommended to use amphotericin B deoxycholate (D-AMB) or its lipid formulations and/or in association with itraconazole (ITC). Our aim was to evaluate the antifungal efficacy of a poly-aggregated amphotericin B (P-AMB), a nonlipid formulation, compared with D-AMB on systemic sporotrichosis caused by Sporothrix brasiliensis. In vitro assays showed that Sporothrix schenckii sensu stricto and S. brasiliensis yeast clinical isolates were susceptible to low concentrations of P-AMB and D-AMB...
June 1, 2017: Medical Mycology: Official Publication of the International Society for Human and Animal Mycology
https://www.readbyqxmd.com/read/28562003/effect-of-alkylation-on-the-cellular-uptake-of-polyethylene-glycol-coated-gold-nanoparticles
#16
Lok Wai Cola Ho, Wing-Yin Yung, Kwun Hei Samuel Sy, Ho Yin Li, Chun Kit K Choi, Ken Cham-Fai Leung, Thomas W Y Lee, Chung Hang Jonathan Choi
Alkyl groups (CnH2n+1) are prevalent in engineered bionanomaterials used for many intracellular applications, yet how alkyl groups dictate the interactions between nanoparticles and mammalian cells remains incomprehensively investigated. In this work, we report the effect of alkylation on the cellular uptake of densely polyethylene glycol-coated nanoparticles, which are characterized by their limited entry into mammalian cells. Specifically, we prepare densely PEGylated gold nanoparticles that bear alkyl chains of varying carbon chain lengths (n) and loading densities (termed "alkyl-PEG-AuNPs"), followed by investigating their uptake by Kera-308 keratinocytes...
June 7, 2017: ACS Nano
https://www.readbyqxmd.com/read/28559542/march9-mediated-ubiquitination-regulates-mhc-i-export-from-the-tgn
#17
Francesca De Angelis Rigotti, Aude De Gassart, Carina Pforr, Florencia Cano, Prudence N'Guessan, Alexis Combes, Voahirana Camossetto, Paul Lehner, Philippe Pierre, Evelina Gatti
Given the heterogeneous nature of antigens, MHC-I intracellular transport intersects with multiple degradation pathways for efficient peptide loading and presentation to cytotoxic T cells. MHC-I loading with peptides in the endoplasmic reticulum (ER) is a tightly regulated process, while post-ER intracellular transport is considered to occur by default, leading to peptide-bearing MHC-I delivery to the plasma membrane. We show here that MHC-I traffic is submitted to a previously uncharacterized sorting step at the trans Golgi network (TGN), dependent on the ubiquitination of its cytoplasmic tail lysine residues...
May 31, 2017: Immunology and Cell Biology
https://www.readbyqxmd.com/read/28559185/novel-dendritic-structure-of-alginate-hybrid-nanoparticles-for-effective-anti-viral-drug-delivery
#18
K S Joshy, Anne George, Jiya Jose, Nandakumar Kalarikkal, Laly A Pothen, Sabu Thomas
Lipid-polymer hybrid nanoparticles have recently gathered much attention as nanoplatforms for drug delivery applications due to their unique structural properties. In this study zidovudine (AZT) loaded hybrid nanoparticles of alginate (ALG) and stearic acid- poly ethylene glycol (SA-PEG) were synthesized. The structural characterization of drug loaded hybrid nanoparticles were studied using FT-IR spectroscopy, DLS and TEM analysis. These hybrid nanoparticles showed dendritic morphology and it can be used as an efficient carrier for zidovudine...
May 27, 2017: International Journal of Biological Macromolecules
https://www.readbyqxmd.com/read/28559042/self-assembled-core-shell-type-lipid-polymer-hybrid-nanoparticles-intracellular-trafficking-and-relevance-for-oral-absorption
#19
Qiuxia Li, Dengning Xia, Jinsong Tao, Aijun Shen, Yuan He, Yong Gan, Chi Wang
Lipid-polymer hybrid nanoparticles (NPs) are advantageous for drug delivery. However, their intracellular trafficking mechanism and relevance for oral drug absorption are poorly understood. In this study, self-assembled core-shell lipid-polymer hybrid NPs made of PLGA and various lipids were developed to study their differing intracellular trafficking in intestinal epithelial cells, and their relevance for oral absorption of a model drug saquinavir (SQV). Our results demonstrated that the endocytosis and exocytosis of hybrid NPs could be changed by varying the kind of lipid...
May 27, 2017: Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28554169/neohesperidin-exerts-lipid-regulating-effects-in-vitro-and-in-vivo-via-fibroblast-growth-factor-21-and-amp-activated-protein-kinase-sirtuin-type-1-peroxisome-proliferator-activated-receptor-gamma-coactivator-1%C3%AE-signaling-axis
#20
Haoshu Wu, Yunxi Liu, Xiaobing Chen, Difeng Zhu, Jian Ma, Youyou Yan, Meimei Si, Xian Li, Chongde Sun, Bo Yang, Qiaojun He, Kunsong Chen
The purpose of this study is to prove the lipid-regulating effects of neohesperidin (NHP) and explore the potential mechanisms related to fibroblast growth factor 21 (FGF21) and AMP-activated protein kinase (AMPK). Free fatty acids (FFAs)-induced lipid-accumulated HepG2 cells, acutely egg yolk-induced dyslipidemia and chronically diet-induced obese (DIO) model mice were treated with NHP. Biochemical analyses were carried out to determine the lipid profiles. Western blotting and real-time PCR were employed to analyze FGF21, AMPK and the related proteins or mRNA expressions...
May 30, 2017: Pharmacology
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